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    MALEIMIDE DERIVATIVES AS MODULATORS OF WNT PATHWAY
    11.
    发明申请
    MALEIMIDE DERIVATIVES AS MODULATORS OF WNT PATHWAY 有权
    作为WNT PATHWAY的调节剂的马来酰亚胺衍生物

    公开(公告)号：US20160318926A1

    公开(公告)日：2016-11-03

    申请号：US15105312

    申请日：2014-12-17

    Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

    Inventor： Jenefer Alam ,  Anders Poulsen ,  Soo Yei Ho ,  Wei Ling Wang ,  Athisayamani Jeyaraj Duraiswamy

    IPC: C07D471/04

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or -alkylaryl; R2 represents H; or alkyl; R3 represents H; or alkyl; U, V and W represent —(CH2)—; or U and V together represent —CH═CH— and W represents C═O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).

    Abstract translation: 本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中R 1表示任选取代的烷基（其中任选的取代基包括一个或多个 取代基，各自独立地选自C 1-6烷氧基）; 任选取代的碳环基（其中任选的取代基包括一个或多个取代基，各自独立地选自C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6卤代烷氧基和卤素）; 或 - 烷基芳基; R2表示H; 或烷基; R3表示H; 或烷基; U，V和W表示 - （CH 2） - ; 或U和V一起表示-CH = CH-，W表示C = O; Y表示芳基; 杂芳基; 任选取代的碳环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6卤代烷氧基和卤素的取代基）。 或任选取代的杂环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，-C（O）OC 1-6烷基，-C（O）C 1-6烷基和-C（O）NHCl -6-烷基）; Z表示芳基; 杂芳基; 任选取代的碳环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6卤代烷氧基和卤素的取代基）。 或任选取代的杂环基（其中任选的取代基包括一个或多个各自独立地选自C 1-6烷基，C 1-6烷氧基，-C（O）OC 1-6烷基，-C（O）C 1-6烷基和-C（O） NHC 1-6烷基）。

    Purine Diones As Wnt Pathway Modulators
    16.
    发明申请
    Purine Diones As Wnt Pathway Modulators 有权
    嘌呤狄更斯作为Wnt途径调节剂

    公开(公告)号：US20160090386A1

    公开(公告)日：2016-03-31

    申请号：US14893172

    申请日：2014-05-19

    Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

    Inventor： Soo Yei Ho ,  Stephanie Eliane Blanchard ,  Athisayamani Jeyaraj Duraiswamy ,  Jenefer Alam ,  Vikrant Arun Adsool

    IPC: C07D473/06 ,  C07D473/08

    CPC classification number: C07D473/06 ,  A61K31/522 ,  A61K31/5377 ,  C07D473/08

    Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.

    Abstract translation: 本发明涉及通用结构（I）化合物在Wnt途径调节中的应用[本文中应该插入其中R 1，R 2，R 3，R 4和R 5各自独立地为H或烷基; D选自H，卤素，烷基，环烷基，芳基和二烷基氨基，每个（H和卤素除外）任选被取代; Ar是任选取代的芳基或杂芳基; Cy是芳基，杂芳基或含有至少一个杂原子的饱和环，各自任选被取代; n为1〜3的整数。

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